| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
ErbB2 10 nM (IC50)
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| ln Vitro |
Insulin receptor, insulin-like growth factor-I receptor, platelet-derived growth factor β, vascular endothelial growth factor 2, Abl, Src, c-Met, JNK-2, JNK-3, ZAP-70, Cdk-2, and Cdk-5 are among the receptors for which CP-724714 is >1,000 times less potent[1]. At concentrations as low as 50 nmol/L (IC50=32 nM), CP-724714 potently inhibits the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain; however, its potency against EGFR is noticeably lower[1]. In vitro, CP-724714 (1 μM; 24 hours) causes G1 cell cycle block in BT-474 human breast carcinoma cells that overexpress erbB2[1].
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| ln Vivo |
ErbB2 receptor phosphorylation is reduced in a concentration-dependent manner by CP-724714 (3.25-100 mg/kg; po; 0.5-8 hours)[1]. CP-724714 (6.25–100 mg/kg; po; qd; for 8–40 days) suppresses the growth of FRE-erbB2 xenografts[1]. Apoptosis is induced in response to CP-724714 (Athymic, female FRE-erbB2 xenograft-bearing mice; 30 or 100 mg/kg; po) in a time- and dose-dependent manner. This was seen as early as 4 to 8 hours following dosing. Eight hours after dose, over 75% more tumor cells in the 100 mg/kg treatment group showed signs of apoptosis than in the vehicle control group. Regression of BT-474 tumors and considerable suppression of several other human tumor xenografts are induced by CP-724714. Furthermore, CP-724714 had no discernible effects on heart tissue and a positive nonclinical toxicity profile[1].
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| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: erbB2-amplified BT-474 breast cancer cells Tested Concentrations: 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Resulted in accumulation of cells in G1 phase and a marked reduction in S-phase cells. |
| Animal Protocol |
Animal/Disease Models: Female athymic mice (bearing FRE-erbB2 xenografts)[1]
Doses: 3.25-100 mg/kg Route of Administration: Po; 0.5-8 hrs (hours) Experimental Results: Produced a reduction of erbB2 tyrosine phosphorylation in FRE-erbB2 xenografts. Animal/Disease Models: Athymic female mice bearing FRE-erbB2 xenografts[1] Doses: 6.25- 100 mg/kg Route of Administration: Po; qd; for 8 to 40 day Experimental Results: Resulted in an inhibition of FRE-erbB2 xenografts. |
| References |
[1]. Jani JP, et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res, 2007, 67(20), 9887-9893.
[2]. Feng B, et al. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicol Sci, 2009, 108(2), 492-500. |
| Molecular Formula |
C27H27N5O3
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|---|---|
| Molecular Weight |
469.53
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| CAS # |
383432-38-0
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| Related CAS # |
(E/Z)-CP-724714;537705-08-1
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| SMILES |
O(C1=C([H])N=C(C([H])([H])[H])C([H])=C1[H])C1C([H])=C([H])C(=C([H])C=1C([H])([H])[H])N([H])C1C2C([H])=C(/C(/[H])=C(\[H])/C([H])([H])N([H])C(C([H])([H])OC([H])([H])[H])=O)C([H])=C([H])C=2N=C([H])N=1
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (106.49 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1298 mL | 10.6489 mL | 21.2979 mL | |
| 5 mM | 0.4260 mL | 2.1298 mL | 4.2596 mL | |
| 10 mM | 0.2130 mL | 1.0649 mL | 2.1298 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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